Compound name
HS38
Protein family
Protein Kinase
Target name
DAPK2
Affinity biochemical (nM)
79
CG-Set
Kinase set
Recommended Concentration
1 µM
Compound EUbOPEN ID
EUB0002103a
SMILES
CC(SC1=NC(N(C2=CC=CC(Cl)=C2)N=C3)=C3C(N1)=O)C(N)=O
InChIKey
NASYEGAVCTZSDO-UHFFFAOYSA-N
NCBI gene ID
23604
UniProt ID
Q9UIK4
Synonyms
DRP-1, MGC119312
Mode of action
Inhibitor
Affinity biochemical definition
Kd
Affinity biochemical assay type
Competition-binding assay (DiscoverX)
Affinity Biochemical Source Knowledge
https://pubmed.ncbi.nlm.nih.gov/24070067/
Affinity biochemical relation
=
Selectivity platform
Kinase panel (Dundee profiling, using a 33P-ATP filter-binding assay)
Selectivity platform number of targets
124
Selectivity remarks
Screened at 10 µM, the closest targets in the screen: DAPK1 (11%), IRAK4 (20%), DYRK2 (21%), PIM1 (23%), PIM3 (24%), CK2 (29%), GCK (43%), PIM2 (64%), smMLCK (71%), ROCK2 (91%), full screening data available as supplemental information, https://pubmed.ncbi.nlm.nih.gov/24070067/;
In-vitro potency (radioactive (33P-ATP) filter-binding assay): IC50(DAPK1) = 200 nM, https://pubmed.ncbi.nlm.nih.gov/24070067/;
In-vitro potency (radioactive (33P-ATP) filter-binding assay): IC50(PIM3) = 200 nM, https://pubmed.ncbi.nlm.nih.gov/24070067/;
In-vitro potency (radioactive (33P-ATP) filter-binding assay): IC50(IRAK4) = 1400 nM, https://pubmed.ncbi.nlm.nih.gov/24070067/;
In-vitro potency (radioactive (33P-ATP) filter-binding assay): IC50(PIM1) = 1700 nM, https://pubmed.ncbi.nlm.nih.gov/24070067/;
In-vitro potency (radioactive (33P-ATP) filter-binding assay): IC50(DYRK2) = 1800 nM, https://pubmed.ncbi.nlm.nih.gov/24070067/;
In-vitro potency (radioactive (33P-ATP) filter-binding assay): IC50(PIM2) = 18000 nM, https://pubmed.ncbi.nlm.nih.gov/24070067/;
In-vitro potency (radioactive (33P-ATP) filter-binding assay): IC50(smMLCK) = 19000 nM, https://pubmed.ncbi.nlm.nih.gov/24070067/;
In-vitro potency (radioactive (33P-ATP) filter-binding assay): IC50(ROCK2) >200000 nM, https://pubmed.ncbi.nlm.nih.gov/24070067/;
In-vitro potency (radioactive (33P-ATP) filter-binding assay): IC50(DAPK1) = 200 nM, https://pubmed.ncbi.nlm.nih.gov/24070067/;
In-vitro potency (radioactive (33P-ATP) filter-binding assay): IC50(PIM3) = 200 nM, https://pubmed.ncbi.nlm.nih.gov/24070067/;
In-vitro potency (radioactive (33P-ATP) filter-binding assay): IC50(IRAK4) = 1400 nM, https://pubmed.ncbi.nlm.nih.gov/24070067/;
In-vitro potency (radioactive (33P-ATP) filter-binding assay): IC50(PIM1) = 1700 nM, https://pubmed.ncbi.nlm.nih.gov/24070067/;
In-vitro potency (radioactive (33P-ATP) filter-binding assay): IC50(DYRK2) = 1800 nM, https://pubmed.ncbi.nlm.nih.gov/24070067/;
In-vitro potency (radioactive (33P-ATP) filter-binding assay): IC50(PIM2) = 18000 nM, https://pubmed.ncbi.nlm.nih.gov/24070067/;
In-vitro potency (radioactive (33P-ATP) filter-binding assay): IC50(smMLCK) = 19000 nM, https://pubmed.ncbi.nlm.nih.gov/24070067/;
In-vitro potency (radioactive (33P-ATP) filter-binding assay): IC50(ROCK2) >200000 nM, https://pubmed.ncbi.nlm.nih.gov/24070067/;
Selectivity Source Knowledge
https://pubmed.ncbi.nlm.nih.gov/24070067/
Selectivity Number of Off-targets
1